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US11478482B2ActiveUtilityPatentIndex 61

Fasudil for the treatment of schizophrenia

Assignee: NATIONAL UNIV CORPORATION TOKAI NATIONAL HIGHER EDUCATION AND RESEARCH SYSTEMPriority: Oct 15, 2018Filed: Jan 31, 2022Granted: Oct 25, 2022
Est. expiryOct 15, 2038(~12.3 yrs left)· nominal 20-yr term from priority
Inventors:OZAKI NORIOYAMADA KIYOFUMINAGAI TAKUMORI DAISUKEARIOKA YukoKUSHIMA Itaru
A61K 31/551A61P 25/18A61P 25/00A61P 43/00A61P 25/24A61K 45/06
61
PatentIndex Score
2
Cited by
10
References
17
Claims

Abstract

The present invention provides an antipsychotic drug comprising fasudil or a pharmaceutically acceptable salt thereof as an active agent for the treatment of schizophrenia, including schizophrenia caused by dysfunction of ARHGAP10.

Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1. A method for the treatment of schizophrenia in a patient in need thereof, wherein the method comprises administering to the patient a therapeutically effective amount of fasudil, or a pharmacologically acceptable salt or hydrate thereof. 
     
     
       2. The method according to  claim 1 , wherein the fasudil, or the pharmacologically acceptable salt or hydrate thereof, is hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine monohydrochloride hemihydrate. 
     
     
       3. The method according to  claim 1 , wherein the method comprises administering to the patient once to several times a day a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       4. The method according to  claim 1 , wherein the method comprises administering to the patient once every two days a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       5. The method according to  claim 1 , wherein the method comprises administering to the patient once every three days a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       6. The method according to  claim 1 , wherein the method comprises orally administering to the patient a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       7. The method according to  claim 1 , wherein the method comprises administering to the patient a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof, in combination with one or more additional active ingredients selected from the group consisting of aripiprazole, asenapine, blonanserin, bromperidol, carpipramine, chlorpromazine, clocapramine, clozapine, fluphenazine, haloperidol, levomepromazine, moperone, mosapramine, nemonapride, olanzapine, paliperidone, perospirone, perphenazine, pimozide, propericiazine, quetiapine, risperidone, spiperone, sulpiride, sultopride, tiapride, and zolpidem. 
     
     
       8. The method according to  claim 1 , wherein the schizophrenia is associated with dysfunction of ARHGAP10. 
     
     
       9. The method according to  claim 8 , wherein the dysfunction of ARHGAP10 is a deletion in the ARHGAP10 gene or a deletion of the ARHGAP10 gene. 
     
     
       10. The method according to  claim 8 , wherein the dysfunction of ARHGAP10 is an amino acid substitution of proline for serine at residue 490 (Ser490Pro). 
     
     
       11. The method according to  claim 8 , wherein the fasudil, or the pharmacologically acceptable salt or hydrate thereof, normalizes dysfunction of ARHGAP10. 
     
     
       12. The method according to  claim 8 , wherein the fasudil, or the pharmacologically acceptable salt or hydrate thereof, is hexahydro-1-(5-isoquinolinesulfonyl)-1H-1,4-diazepine monohydrochloride hemihydrate. 
     
     
       13. The method according to  claim 8 , wherein the method comprises administering to the patient once to several times a day a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       14. The method according to  claim 8 , wherein the method comprises administering to the patient once every two days a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       15. The method according to  claim 8 , wherein the method comprises administering to the patient once every three days a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       16. The method according to  claim 8 , wherein the method comprises orally administering to the patient a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof. 
     
     
       17. The method according to  claim 8 , wherein the method comprises administering to the patient a therapeutically effective amount of the fasudil, or the pharmacologically acceptable salt or hydrate thereof, in combination with one or more additional active ingredients selected from the group consisting of aripiprazole, asenapine, blonanserin, bromperidol, carpipramine, chlorpromazine, clocapramine, clozapine, fluphenazine, haloperidol, levomepromazine, moperone, mosapramine, nemonapride, olanzapine, paliperidone, perospirone, perphenazine, pimozide, propericiazine, quetiapine, risperidone, spiperone, sulpiride, sultopride, tiapride, and zolpidem.

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